Sustained release formulation of a non-steroidal anti-inflammatory drug

Patent metadata

Field	Value
Publication number	US-9974744-B2
Application number	US-201313787265-A
Country	US
Kind code	B2
Filing date	Mar 6, 2013
Priority date	Oct 28, 2010
Publication date	May 22, 2018
Grant date	May 22, 2018

Abstract

Disclosed are formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs which minimize the side effects of unencapsulated non-steroidal anti-inflammatory drugs while maintaining or improving efficacy. Methods of making and administering the formulations comprising multivesicular liposomes and one or more non-steroidal anti-inflammatory drugs and their use as medicaments are also provided.

First claim

What is claimed is:

1. A method of treating pain and inflammation, comprising administering a formulation comprising one or more non-steroidal anti-inflammatory drugs encapsulated in a first aqueous phase of multivesicular liposomes, to a subject in need thereof by injection, wherein the multivesicular liposomes comprise at least one anionic amphipathic phospholipid and at least one neutral lipid, wherein the one or more non-steroidal anti-inflammatory drugs are selected from the group consisting of meloxicam, piroxicam, and diclofenac, and wherein the total concentration of the non-steroidal anti-inflammatory drug in the multivesicular liposomes formulation is at least about 1.0 mg/mL.

2. The method of claim 1 , wherein the formulation further comprises a pharmaceutically acceptable carrier for injection.

3. The method of claim 1 , wherein the multivesicular liposomes comprise cholesterol, one or more phosphatidylglycerols, including salts of the phosphatidylglycerols, and one or more triglycerides.

4. The method of claim 1 , wherein the multivesicular liposomes comprise DPPG, DEPC, and tricaprylin.

5. The method of claim 1 , wherein the multivesicular liposomes comprise lysine.

6. The method of claim 1 , wherein the multivesicular liposomes comprise glutamic acid.

7. The method of claim 1 , wherein said administration is subcutaneous injection.

8. The method of claim 1 , wherein said administration is intramuscular injection.

9. The method of claim 1 , wherein said administration is intraarticular injection.

10. The method of claim 1 , wherein said administration comprises wound infiltration by local injection into a wound margin.

11. The method of claim 1 , wherein administration is every 1 to 7 days.

12. The method of claim 1 , wherein said non-steroidal anti-inflammatory drug is diclofenac.

13. The method of claim 1 , wherein said non-steroidal anti-inflammatory drug is meloxicam.

14. The method of claim 1 , wherein said multivesicular liposomes comprise a pH modifier selected from the group consisting of an inorganic acid, an inorganic base, an organic acid, an organic base, and a combination thereof.

15. The method of claim 1 , wherein said non-steroidal anti-inflammatory drug is piroxicam.

16. The method of claim 1 , wherein said multivesicular liposomes are characterized by an internal pH of about 8 to about 9.

17. The method of claim 1 , wherein said multivesicular liposomes comprise a pH modifier in the first aqueous phase selected from the group consisting of an organic acid, an organic base, and a combination thereof.

18. The method of claim 17 , wherein said multivesicular liposomes comprise an organic acid.

19. The method of claim 17 , wherein said multivesicular liposomes comprise an organic base.

20. The method of claim 1 , wherein said administration comprises instillation into a wound.

Assignees

• Pacira Pharmaceuticals Inc

Inventors

• Garcia Louie Daniel
• Zhu Liangjin
• Lambert William Joseph
• Patou Gary

Classifications

• A61P25/04

  Centrally acting analgesics, e.g. opioids · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

• A61K31/196

  the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil · CPC title

• A61K9/127

  Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant · CPC title

• A61K31/5415

  ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam · CPC title